Buspiron

Bezeichnung:Buspiron

CAS-Nr36505-84-7

Englisch Name:Buspirone

CBNumberCB1367137

SummenformelC21H31N5O2

Molgewicht385.5

MOL-Datei36505-84-7.mol

Synonyma

Buspiron

Buspiron physikalisch-chemischer Eigenschaften

Schmelzpunkt	105-107 °C(Solv: ethyl acetate (141-78-6))
Siedepunkt	511.93°C (rough estimate)
Dichte	1.1527 (rough estimate)
Brechungsindex	1.7600 (estimate)
storage temp.	Sealed in dry,2-8°C
pka	pKa 7.60±0.01(H2O t=25.0 I=0.1(NaCl)) (Uncertain)
Aggregatzustand	Solid
Farbe	White to off-white
BCS Class	1
CAS Datenbank	36505-84-7(CAS DataBase Reference)
NIST chemische Informationen	8-Azaspiro[4.5]decane-7,9-dione, 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-(36505-84-7)
EPA chemische Informationen	8-Azaspiro[4.5]decane-7,9-dione, 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]- (36505-84-7)

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	45
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
RTECS-Nr.	CL9915000

Gefahreninformationscode (GHS)

Buspirone Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R25:Giftig beim Verschlucken.
S-Sätze Betriebsanweisung:
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Verwenden
Tranquilizer (minor).
Verwenden
5-Chloro Buspirone is an impurity of Buspirone Hydrochloride (B689850), a non-benzodiazepine anxiolytic and a 5-hydroxytryptamine (5-HT1) receptor agonist.
Verwenden
Buspirone is an extremely specific drug that could possibly represent a new chemical class of anxiolytics—azaspirones. As an anxiolytic, its activity is equal to that of benzodiazepines; however, it is devoid of anticonvulsant and muscle relaxant properties, which are characteristic of benzodiazepines.
Definition
ChEBI: An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N4 position.
Trademarks
Buspar (Bristol-Myers Squibb).
Biologische Funktion
Buspirone (BuSpar) is the first example of a class of anxiolytic agents that can relieve some symptoms of anxiety in doses that do not cause sedation. Buspirone is structurally unrelated to existing psychotropic drugs.
Allgemeine Beschreibung
The initial compound in this series, buspirone (BuSpar), hasanxiolytic and antidepressant activities and is a partial5-HT_1A agonist. Its anxiolytic activity is reportedly causedby its ability to diminish 5-HT release (via 5-HT_1A agonism).High short-term synaptic levels of 5-HT are characteristic ofanxiety. Also, because it is a partial agonist, it can stimulatepostsynaptic receptors when 5-HT levels are low in thesynapse, as is the case in depression. Several other spironesare in development as anxiolytics and antidepressants.
Mechanism of action
Although buspirone has been shown to interact with a number of neurotransmitter systems in the brain, it appears that its clinically relevant effects are mediated through interactions at the serotonin (5-hydroxytryptamine, 5-HT) 5-HT_1A receptor, where it acts as a partial agonist.
Pharmakologie
Buspirone is as effective as the benzodiazepines in the treatment of general anxiety. However, the full anxiolytic effect of buspirone takes several weeks to develop, whereas the anxiolytic effect of the benzodiazepines is maximal after a few days of therapy. In therapeutic doses, buspirone has little or no sedative effect and lacks the muscle relaxant and anticonvulsant properties of the benzodiazepines. In addition, buspirone does not potentiate the central nervous system depression caused by sedative–hypnotic drugs or by alcohol, and it does not prevent the symptoms associated with benzodiazepine withdrawal.
Clinical Use
Buspirone is effective in general anxiety and in anxiety with depression.
Nebenwirkungen
Like the benzodiazepines, buspirone appears to be safe even when given in very high doses. The most common side effects are dizziness, light-headedness, and headache. Abuse, dependence, and withdrawal have not been reported, and buspirone administration does not produce any cross-tolerance to the benzodiazepines. Buspirone has been reported to increase blood pressure in patients taking monoamine oxidase inhibitors, and it may increase plasma levels of haloperidol if coadministered with that agent.
Synthese
Buspirone, 8-[4-[4-(2-pyrimidyl)-1-piperazinyl]butyl]-8-azaspiro [4,5] decan-7,9-dione (5.2.6), is synthesized by the reaction of 1-(2-pyrimidyl)-4- (4-aminobutyl)piperazine (5.2.4) with 8-oxaspiro[4,5]decan-7,9-dione (5.2.5). In turn, 1- (2-pyrimidyl)-4-(4-aminobutyl)piperazine (5.2.4) is synthesized by the reaction of 1-(2-pyrimidyl)piperazine with 4-chlorobutyronitrile, giving 4-(2-pyrimidyl)-1-(3- cyanopropyl)piperazine (5.2.3), which is hydrogenated with Raney nickel into buspirone (5.2.4) [51¨C55].
Stoffwechsel
Buspirone is well absorbed from the gastrointestinal tract, and peak blood levels are achieved in 1 to 1.5 hours; the drug is more than 95% bound to plasma proteins. Buspirone is extensively metabolized, with less than 1% of the parent drug excreted into the urine unchanged. At least one of the metabolic products of buspirone is biologically active. The parent drug has an elimination half-life of 4 to 6 hours.

Buspirone Upstream-Materialien And Downstream Produkte

Buspiron Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

36505-84-7, Buspirone Verwandte Suche:

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